Abstract:
:A novel cosalane analog having an extended polyanionic pharmacophore was synthesized in order to target specific cationic residues on the surface of CD4. The design rationale is based on a hypothetical binding model of cosalane to the surface of the protein. The new analog displayed an EC50 of 0.55 microM as an inhibitor of the cytopathic effect of HIV-1RF in CEM-SS cells, which represents a significant increase in potency over cosalane itself (EC50 5.1 microM). Both cosalane and the new analog are inhibitors of viral entry into target cells.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Cushman M,Insaf S,Ruell JA,Schaeffer CA,Rice WGdoi
10.1016/s0960-894x(98)00121-8subject
Has Abstractpub_date
1998-04-07 00:00:00pages
833-6issue
7eissn
0960-894Xissn
1464-3405pii
S0960-894X(98)00121-8journal_volume
8pub_type
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